5-Butyl-1H-pyrazole-3-carboxylic acid

Description

LUF6283 is a partial agonist of GPR109A/HCA₂ G protein-coupled receptors (K_i = 0.55 μM in a radioligand binding assay). It stimulates [³⁵S]-GTPγS binding and increases phosphorylation of ERK in HEK293T cells expressing GPR109A/HCA₂ receptors (EC₅₀s = 3.1 and 0.32 μM, respectively). In vivo, LUF6283 (400 mg/kg per day) reduces plasma levels of VLDL and hepatic expression of apolipoprotein B in mice.

Uses

LUF 6283 is a partial agonist of HCA2 and is a promising drug candidate to achieve a beneficial lipid lowering effect of niacin, ultimately treating dyslipidemic disorders.